JH-XI-10-02

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19[1].

Product Specifications

CAS Number

[2209085-22-1]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

CDK; PROTACs

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/JH-XI-10-02.html

Purity

99.73

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N([C@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)[C@@H](C5=CC6=C(C=C5)C=CN=C6)CC[C@@]4([H])[C@]3([H])CC[C@@]2([H])C1)C)CCOCCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O

Molecular Formula

C53H69N5O9

Molecular Weight

920.14

Precautions

H315, H319, H320

References & Citations

[1]Hatcher JM, et al. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Mar 18;9 (6) :540-545.